Assay Detail
Binding
CHEMBL3875323
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Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling activity using relaxed pBR322 as substrate incubated for 30 mins in presence of ATP by ethidium bromide staining based agarose gel electrophoresis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mycobacterium tuberculosis |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
DNA gyrase subunit A/DNA gyrase subunit B (CHEMBL3430898) ↗| Type | PROTEIN COMPLEX |
| Organism | Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv) |
Publication
Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.41 | 4.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL242550 | DIOSPYRIN | — | 1 | 4.82 |
| CHEMBL430853 | RAMENTACEONE | — | 1 | 4.52 |
| CHEMBL241392 | NEODIOSPYRIN | — | 1 | 4.30 |
| CHEMBL1992900 | — | — | 1 | 4.00 |
| CHEMBL590 | MENADIONE | 4.0 | 1 | - |
| CHEMBL3884255 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL242550 | DIOSPYRIN | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL430853 | RAMENTACEONE | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL241392 | NEODIOSPYRIN | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL1992900 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL590 | MENADIONE | IC50 | > | 200000.0 | nM | - |
| CHEMBL3884255 | — | IC50 | > | 200000.0 | nM | - |